I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH

I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH

Isicelo socwaningo:
Le nhlanganisela iyi-derivative ye-lysine evikelwe, esebenzayo esetshenziswa ekuhlanganiseni kwe-peptide nasekuthuthukisweni kwe-conjugate yezidakamizwa. Ihlanganisa iqembu le-Fmoc lokuvikela i-N-terminal, kanye nokuguqulwa kwe-side-chain nge-Eic(OtBu) (i-eicosanoic acid derivative), γ-glutamic acid (γ-Glu), kanye ne-AEEA (aminoethoxyethoxyacetate). Lezi zingxenye zenzelwe ukutadisha imiphumela ye-lipidation, i-spacer chemistry, nokukhululwa kwezidakamizwa okulawulwayo. Icwaningwa kabanzi kumongo wamasu we-prodrug, izixhumanisi ze-ADC, nama-peptide asebenzisana nolwelwesi.

Umsebenzi:
I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH isebenza njengesakhiwo sokwakha ama-peptide ashintshwe i-lipid noma amasistimu okulethwa kwezidakamizwa. I-Eic moiety ithuthukisa i-lipophilicity kanye nokubopha ulwelwesi; I-γ-Glu yengeza ukuzinza kwe-enzymatic namandla okukhomba; futhi i-AEEA isebenza njengesixhumi esiguquguqukayo se-hydrophilic. Ndawonye, ​​anika amandla ukwakhiwa kwama-peptide ngokuthathwa kwamaselula okuthuthukisiwe, uhhafu wempilo eyandisiwe, kanye nezindawo zokulethwa eziqondene nesayithi.